Radiopharmacokinetic and dosimetric parameters of 188Re-lanreotide in athymic mice with induced human cancer tumors

Molina-Trinidad, Eva María; Murphy, Consuelo Arteaga de; Ferro-Flores, Guillermina; Murphy-Stack, Eduardo; Jung‐Cook, Helgi

doi:10.1016/j.ijpharm.2005.11.043

Cited by 27 publications

(9 citation statements)

References 12 publications

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“…The encouraging clinical applications of labeled somatostatin analogues as therapeutic modality in somatostatin receptor-positive lesions have been reported. It has reduced the tumor growth by metastasis instudies where radiopharmaceuticals are used; a better quality of life by controling the symptoms and a larger survival of patients [19][20][21][22][23][24][25][26][27][28][40][41][42][43][44][45][46][47][48] . Have been shown it is known that adenomas and various tumors of neuroendocrine origin are over expressed in somatostatin receptors.…”

Section: Resultsmentioning

confidence: 99%

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2015

IJPSR

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The Ooctapéptido (LAN: 3-(2-Naphthalenyl)-D-alanyl-L-cysteinyl-L-tyrosyl-Dtryptophyl-L-lysyl-L-valyl-L-cysteinyl-L-threoninamide (2 → 7) disulphide acetate, angiopeptin acetate) cyclic covered gold nanoparticles (AuNPs) results in a complex (AuNPs-LAN) when reacted following the aqueous synthesis using Turkevich method for preparing colloidal gold nanoparticles followed by reaction of conjugation with the octapeptide LAN. The nanoconjugate was characterized by transmission electron microscopy high-resolution, UV-vis spectrophotometry, and by Zeta-potential. The objective of this study was to develop a method of capillary zone electrophoresis (CZE) to determine AuNPs and AuNPs-LAN in vitro. The reaction was I carried out by reduction of HAuCl4 with trisodium citrate, based on the synthesis of Turkevich-Frens-Kimling for colloidal Au at 90 °C where the plasmon resonance was detected at a wavelength of 526 nm, previously reported from 1954, 1976 and 2006, wavelength UV-vis nanoconjugate was 531 nm in which prolongation observed in migration times. We also describe part of the validation (linearity and precision) by capillary electrophoresis, arguing that it is a suitable method to quantify the gold nanoparticles and AuNPs-LAN complex. We conclude that the CZE has greater sensitivity to determine AuNPs and AuNP-LAN, comparing to the method described by UV-Vis spectrophotometry, resulting in a good method for analysis and characterization of the nanoparticles and the conjugated compound. HRTEM necessary to use also is important to know the identification and characterization of these compounds to quantify them in biological fluids for biodistribution and pharmacokinetic studies.

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Section: Resultsmentioning

confidence: 99%

“…The LAN is constituted by eight amino acids which are held together by an internal disulfide crosslink (Cys-Cys). The somatostatin analogue peptide was used for peptide-mediated therapy receiver metastatic neuroendocrine tumors [18][19][20] .…”

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confidence: 99%

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2015

IJPSR

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“…The relative organ mass scaling method was employed to extrapolate the animal data to humans [24, 25]. The mean absorbed dose in various tissues was calculated from the radionuclide concentration in tissues/organs of interest, assuming a homogeneous distribution of the radionuclide within any source region [26].…”

Section: Methodsmentioning

confidence: 99%

Molecular Imaging, Pharmacokinetics, and Dosimetry of¹¹¹In-AMBA in Human Prostate Tumor-Bearing Mice

Liu

et al. 2011

Journal of Biomedicine and Biotechnology

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Molecular imaging with promise of personalized medicine can provide patient-specific information noninvasively, thus enabling treatment to be tailored to the specific biological attributes of both the disease and the patient. This study was to investigate the characterization of DO3A-CH2CO-G-4-aminobenzoyl-Q-W-A-V-G-H-L-M-NH2 (AMBA) in vitro, MicroSPECT/CT imaging, and biological activities of 111In-AMBA in PC-3 prostate tumor-bearing SCID mice. The uptake of 111In-AMBA reached highest with 3.87 ± 0.65% ID/g at 8 h. MicroSPECT/CT imaging studies suggested that the uptake of 111In-AMBA was clearly visualized between 8 and 48 h postinjection. The distribution half-life (t1/2α) and the elimination half-life (t1/2β) of 111In-AMBA in mice were 1.53 h and 30.7 h, respectively. The Cmax and AUC of 111In-AMBA were 7.57% ID/g and 66.39 h∗% ID/g, respectively. The effective dose appeared to be 0.11 mSv/MBq−1. We demonstrated a good uptake of 111In-AMBA in the GRPR-overexpressed PC-3 tumor-bearing SCID mice. 111In-AMBA is a safe, potential molecular image-guided diagnostic agent for human GRPR-positive tumors, ranging from simple and straightforward biodistribution studies to improve the efficacy of combined modality anticancer therapy.

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“…Attaching radionuclides to treatments such as SSAs results in radiolabeled peptides that allow increased radiation exposure in tumor cells versus normal tissue [48]. In a radiopharmacokinetic and dosimetric preclinical study on the lanreotide peptide, radiolabeled rhenium ( 188 Re) was attached to lanreotide via a direct labeling method.…”

Section: Key Preclinical Datamentioning

confidence: 99%

Lanreotide for the treatment of gastroenteropancreatic neuroendocrine tumors

Saif

2016

Expert Opinion on Pharmacotherapy

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The role of SSAs in NET treatment was historically one of symptom management. Although this is a critical therapeutic component, ideal treatment would include prevention of tumor progression. As GEP-NETs are biologically diverse, progression prevention can be difficult, depending on primary tumor site and functional status. Recent data indicate that lanreotide significantly prolonged progression-free survival in metastatic GEP-NET patients. Practice patterns seem to be shifting toward using SSAs as first-line therapy. Response to SSAs has typically been categorized as either symptomatic or biochemical. However, SSA use to prevent tumor progression will lead to a new, objective response category based on tumor growth.

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Radiopharmacokinetic and dosimetric parameters of 188Re-lanreotide in athymic mice with induced human cancer tumors

Cited by 27 publications

References 12 publications

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Molecular Imaging, Pharmacokinetics, and Dosimetry of¹¹¹In-AMBA in Human Prostate Tumor-Bearing Mice

Lanreotide for the treatment of gastroenteropancreatic neuroendocrine tumors

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Radiopharmacokinetic and dosimetric parameters of 188Re-lanreotide in athymic mice with induced human cancer tumors

Cited by 27 publications

References 12 publications

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Molecular Imaging, Pharmacokinetics, and Dosimetry of111In-AMBA in Human Prostate Tumor-Bearing Mice

Lanreotide for the treatment of gastroenteropancreatic neuroendocrine tumors

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Molecular Imaging, Pharmacokinetics, and Dosimetry of¹¹¹In-AMBA in Human Prostate Tumor-Bearing Mice